871266-63-6

871266-63-6 structure

Name: PCI-27483
Chemical Name: L-Aspartic acid, N-[2-[5-[6-(aminoiminomethyl)-1H-benzimidazol-2-yl]-5'-(aminosulfonyl)-2',6-dihydroxy[1,1'-biphenyl]-3-yl]acetyl]
CAS Number: 871266-63-6
Molecular Formula: C₂₆H₂₄N₆O₉S
Molecular Weight: 596.569
Catalog: Research Areas Cancer
Create Date: 2017-05-23 17:01:40
Modify Date: 2024-01-06 18:16:14
PCI-27483 is a FVIIa/tissue factor inhibitor, with antitumour effects.

Name	L-Aspartic acid, N-[2-[5-[6-(aminoiminomethyl)-1H-benzimidazol-2-yl]-5'-(aminosulfonyl)-2',6-dihydroxy[1,1'-biphenyl]-3-yl]acetyl]
Synonyms	L-Aspartic acid, N-[2-[5-[6-(aminoiminomethyl)-1H-benzimidazol-2-yl]-5'-(aminosulfonyl)-2',6-dihydroxy[1,1'-biphenyl]-3-yl]acetyl]- L-Aspartic acid, N-[[5-[5-(aminoiminomethyl)-1H-benzimidazol-2-yl]-5'-(aminosulfonyl)-2',6-dihydroxy[1,1'-biphenyl]-3-yl]acetyl]- (S)-2-[[2-[5-(5-Carbamimidoyl-1H-benzimidazol-2-yl)-6,2'-dihydroxy-5'-sulfamoylbiphenyl-3-yl]acetyl]amino]succinic acid PCI27483/PCI-27483 N-{[5-(5-Carbamimidoyl-1H-benzimidazol-2-yl)-2',6-dihydroxy-5'-sulfamoyl-3-biphenylyl]acetyl}-L-aspartic acid PCI-27483

Description	PCI-27483 is a FVIIa/tissue factor inhibitor, with antitumour effects.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Cancer
In Vitro	PCI-27483 inhibits the TF:FVIIa-complex induced phosphorylation of ERK1/2 and subsequent induction of c-fos in BxPC3 cells, a human pancreatic adenocarcinoma line that highly expresses TF. Furthermore, PCI-27483 blocks the TF:FVIIa induced secretion of IL8 in both BxPC3 cells and MDA-MB-231 breast cancer cells[2].
In Vivo	PCI-27483 shows dose-dependent inhibition of thrombus formation, fibrin accumulation and PT. PCI-27483 (4 mg/kg) shows comparable anticoagulation effects as 2 mg/kg enoxaparin[1]. PCI-27483 (0 and 90 mg/kg, s.c.) results in inhibition of tumor growth in CD1 nu/nu mice implanted with BxPC3 cells[2].
References	[1]. Gómez-Outes A, et al. New parenteral anticoagulants in development. Ther Adv Cardiovasc Dis. 2011 Feb;5(1):33-59. [2]. Julia Prescott, et al. PCI-27483, a small molecule inhibitor of Factor VIIa, inhibits growth of BxPC3 pancreatic adenocarcinoma xenograft tumors. Cancer Research May 2008 Volume 68, Issue 9 Supplement.